A short and efficient synthesis of valsartan via a Negishi reaction

An efficient synthesis of the angiotensin-II inhibitor valsartan (Diovan®) is presented. Directed ortho-metalation of 5-phenyl-1-trityl-1H-tetrazole (6) and its Negishi coupling with aryl bromide 5 are the key steps of the synthesis. This method overcomes many of the drawbacks associated with previo...

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Main Authors:	Samir Ghosh, A. Sanjeev Kumar, G. N. Mehta
Format:	Article
Language:	English
Published:	Beilstein-Institut 2010-03-01
Series:	Beilstein Journal of Organic Chemistry
Subjects:	antihypertensive therapy aryl bromide Negishi coupling tetrazole valsartan
Online Access:	https://doi.org/10.3762/bjoc.6.27

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spelling	doaj-dda6d6fdc5854146ade18307d31d5b632021-02-02T01:53:31ZengBeilstein-InstitutBeilstein Journal of Organic Chemistry1860-53972010-03-01612710.3762/bjoc.6.271860-5397-6-27A short and efficient synthesis of valsartan via a Negishi reactionSamir Ghosh0A. Sanjeev Kumar1G. N. Mehta2Applied Chemistry Department, S.V. National Institute of Technology, Surat-395 007, IndiaApplied Chemistry Department, S.V. National Institute of Technology, Surat-395 007, IndiaApplied Chemistry Department, S.V. National Institute of Technology, Surat-395 007, IndiaAn efficient synthesis of the angiotensin-II inhibitor valsartan (Diovan®) is presented. Directed ortho-metalation of 5-phenyl-1-trityl-1H-tetrazole (6) and its Negishi coupling with aryl bromide 5 are the key steps of the synthesis. This method overcomes many of the drawbacks associated with previously reported syntheses.https://doi.org/10.3762/bjoc.6.27antihypertensive therapyaryl bromideNegishi couplingtetrazolevalsartan
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Samir Ghosh A. Sanjeev Kumar G. N. Mehta
spellingShingle	Samir Ghosh A. Sanjeev Kumar G. N. Mehta A short and efficient synthesis of valsartan via a Negishi reaction Beilstein Journal of Organic Chemistry antihypertensive therapy aryl bromide Negishi coupling tetrazole valsartan
author_facet	Samir Ghosh A. Sanjeev Kumar G. N. Mehta
author_sort	Samir Ghosh
title	A short and efficient synthesis of valsartan via a Negishi reaction
title_short	A short and efficient synthesis of valsartan via a Negishi reaction
title_full	A short and efficient synthesis of valsartan via a Negishi reaction
title_fullStr	A short and efficient synthesis of valsartan via a Negishi reaction
title_full_unstemmed	A short and efficient synthesis of valsartan via a Negishi reaction
title_sort	short and efficient synthesis of valsartan via a negishi reaction
publisher	Beilstein-Institut
series	Beilstein Journal of Organic Chemistry
issn	1860-5397
publishDate	2010-03-01
description	An efficient synthesis of the angiotensin-II inhibitor valsartan (Diovan®) is presented. Directed ortho-metalation of 5-phenyl-1-trityl-1H-tetrazole (6) and its Negishi coupling with aryl bromide 5 are the key steps of the synthesis. This method overcomes many of the drawbacks associated with previously reported syntheses.
topic	antihypertensive therapy aryl bromide Negishi coupling tetrazole valsartan
url	https://doi.org/10.3762/bjoc.6.27
work_keys_str_mv	AT samirghosh ashortandefficientsynthesisofvalsartanviaanegishireaction AT asanjeevkumar ashortandefficientsynthesisofvalsartanviaanegishireaction AT gnmehta ashortandefficientsynthesisofvalsartanviaanegishireaction AT samirghosh shortandefficientsynthesisofvalsartanviaanegishireaction AT asanjeevkumar shortandefficientsynthesisofvalsartanviaanegishireaction AT gnmehta shortandefficientsynthesisofvalsartanviaanegishireaction
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A short and efficient synthesis of valsartan via a Negishi reaction

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